NZ554619A - Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 CGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women - Google Patents
Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 CGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal womenInfo
- Publication number
- NZ554619A NZ554619A NZ554619A NZ55461905A NZ554619A NZ 554619 A NZ554619 A NZ 554619A NZ 554619 A NZ554619 A NZ 554619A NZ 55461905 A NZ55461905 A NZ 55461905A NZ 554619 A NZ554619 A NZ 554619A
- Authority
- NZ
- New Zealand
- Prior art keywords
- vaginal
- acid
- group
- layer
- atrophy
- Prior art date
Links
- 239000000333 selective estrogen receptor modulator Substances 0.000 title claims abstract description 84
- 229940095743 selective estrogen receptor modulator Drugs 0.000 title claims abstract description 68
- 239000003163 gonadal steroid hormone Substances 0.000 title claims abstract description 36
- 239000002243 precursor Substances 0.000 title claims abstract description 36
- 201000001880 Sexual dysfunction Diseases 0.000 title claims abstract description 25
- 231100000872 sexual dysfunction Toxicity 0.000 title claims abstract description 25
- 238000011282 treatment Methods 0.000 title description 40
- 229940011871 estrogen Drugs 0.000 title description 25
- 239000000262 estrogen Substances 0.000 title description 25
- 206010047791 Vulvovaginal dryness Diseases 0.000 title description 11
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 title description 10
- 239000002571 phosphodiesterase inhibitor Substances 0.000 title description 10
- 230000002265 prevention Effects 0.000 title description 3
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims abstract description 203
- FMGSKLZLMKYGDP-UHFFFAOYSA-N Dehydroepiandrosterone Natural products C1C(O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 FMGSKLZLMKYGDP-UHFFFAOYSA-N 0.000 claims abstract description 197
- 229960002847 prasterone Drugs 0.000 claims abstract description 197
- 210000001215 vagina Anatomy 0.000 claims abstract description 69
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- 206010003694 Atrophy Diseases 0.000 claims abstract description 52
- 230000037444 atrophy Effects 0.000 claims abstract description 52
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- 229920001436 collagen Polymers 0.000 claims abstract description 29
- 239000003814 drug Substances 0.000 claims abstract description 29
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- 208000004483 Dyspareunia Diseases 0.000 claims abstract description 21
- CZWCKYRVOZZJNM-UHFFFAOYSA-N Prasterone sodium sulfate Natural products C1C(OS(O)(=O)=O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 CZWCKYRVOZZJNM-UHFFFAOYSA-N 0.000 claims abstract description 21
- CZWCKYRVOZZJNM-USOAJAOKSA-N dehydroepiandrosterone sulfate Chemical compound C1[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 CZWCKYRVOZZJNM-USOAJAOKSA-N 0.000 claims abstract description 21
- 229950009829 prasterone sulfate Drugs 0.000 claims abstract description 21
- 208000004746 Atrophic Vaginitis Diseases 0.000 claims abstract description 20
- 206010003693 Atrophic vulvovaginitis Diseases 0.000 claims abstract description 20
- 201000010808 postmenopausal atrophic vaginitis Diseases 0.000 claims abstract description 20
- 208000013464 vaginal disease Diseases 0.000 claims abstract description 19
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- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 claims abstract 4
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- DUYNJNWVGIWJRI-LJAQVGFWSA-N acolbifene Chemical group C1=CC([C@H]2C(=C(C3=CC=C(O)C=C3O2)C)C=2C=CC(O)=CC=2)=CC=C1OCCN1CCCCC1 DUYNJNWVGIWJRI-LJAQVGFWSA-N 0.000 claims description 103
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- 125000003118 aryl group Chemical group 0.000 claims description 15
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- 238000002648 combination therapy Methods 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
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- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 6
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- 125000005843 halogen group Chemical group 0.000 claims description 6
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 6
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Classifications
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- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
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- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62045204P | 2004-10-20 | 2004-10-20 | |
| PCT/CA2005/001612 WO2006042409A1 (fr) | 2004-10-20 | 2005-10-20 | Precurseurs de steroide sexuel, seuls ou combines a un modulateur de recepteur d'oestrogene selectif et/ou a des oestrogenes et/ou a un inhibiteur de phosphodiesterase de type 5 cgmp, pour prevenir et traiter la secheresse vaginale et les dysfonctionnements sexuels chez la femme postmenopausee |
Publications (1)
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| NZ554619A true NZ554619A (en) | 2011-01-28 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| NZ554619A NZ554619A (en) | 2004-10-20 | 2005-10-20 | Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 CGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women |
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| EP (1) | EP1802312B1 (fr) |
| JP (3) | JP5057983B2 (fr) |
| KR (1) | KR20070067235A (fr) |
| CN (5) | CN102357248A (fr) |
| AP (1) | AP2365A (fr) |
| AU (1) | AU2005297367B2 (fr) |
| BR (1) | BRPI0516243C1 (fr) |
| CA (2) | CA2584524C (fr) |
| DK (1) | DK1802312T3 (fr) |
| EA (1) | EA014878B1 (fr) |
| ES (1) | ES2553101T3 (fr) |
| GE (1) | GEP20105066B (fr) |
| HK (1) | HK1225629A1 (fr) |
| HR (1) | HRP20070169B1 (fr) |
| HU (1) | HUE025651T2 (fr) |
| IL (3) | IL182633A (fr) |
| MA (1) | MA29018B1 (fr) |
| MX (3) | MX2007004830A (fr) |
| NO (1) | NO340123B1 (fr) |
| NZ (1) | NZ554619A (fr) |
| RS (1) | RS20070166A (fr) |
| SG (2) | SG155258A1 (fr) |
| TN (1) | TNSN07147A1 (fr) |
| UA (1) | UA93985C2 (fr) |
| WO (1) | WO2006042409A1 (fr) |
| ZA (1) | ZA200703198B (fr) |
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| US6465445B1 (en) * | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| ES2553101T3 (es) * | 2004-10-20 | 2015-12-04 | Endorecherche Inc. | Precursor de esteroides sexuales en combinación con un modulador selectivo del receptor de estrógenos para la prevención y tratamiento de atrofia vaginal en mujeres postmenopáusicas |
| CA2654152A1 (fr) * | 2006-06-02 | 2007-12-13 | Pear Tree Women's Health Care | Procede de traitement de la vaginite atrophique |
| US20080312239A1 (en) * | 2007-06-13 | 2008-12-18 | Quatrx Pharmaceuticals Company | Methods for the treatment of erectile dysfunction using fispemifene |
| EP2011496A1 (fr) * | 2007-07-03 | 2009-01-07 | Indena S.P.A. | Combinaisons de substances vasoactives avec des estrogènes et leur utilisation dans le traitement de dysfonctionnements sexuels chez les femmes |
| US8268806B2 (en) * | 2007-08-10 | 2012-09-18 | Endorecherche, Inc. | Pharmaceutical compositions |
| AU2012204083C1 (en) * | 2007-08-10 | 2015-02-05 | Myriel Pharmaceuticals, Llc | DHEA compositions for treating menopause |
| AU2014201406B2 (en) * | 2009-06-16 | 2016-08-11 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
| US20100317635A1 (en) * | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
| US8703810B2 (en) | 2010-06-10 | 2014-04-22 | Seragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| KR20140089402A (ko) | 2010-06-16 | 2014-07-14 | 앙도르쉐르슈 인코포레이티드 | 에스트로겐-관련 질병의 치료 또는 예방 방법 |
| US20130231317A1 (en) * | 2011-07-19 | 2013-09-05 | Michael S. Riepl | Dhea bioadhesive controlled release gel |
| US9320744B2 (en) | 2011-10-19 | 2016-04-26 | Dhea Llc | DHEA bioadhesive controlled release gel |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| PT2782584T (pt) | 2011-11-23 | 2021-09-02 | Therapeuticsmd Inc | Preparações e terapias de substituição para hormonoterapias naturais combinadas |
| AU2012351942B2 (en) | 2011-12-14 | 2017-07-06 | Seragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
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| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US20140045806A1 (en) * | 2012-07-25 | 2014-02-13 | Fernand Labrie | Sexual arousal, sexual desire, orgasm and/or pleasure following intravaginal prasterone (dhea) administration in women not suffering or independently from dyspareunia or other symptoms of vulvo-vaginal atrophy |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
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| MX2018006882A (es) * | 2015-12-07 | 2019-05-16 | Therapeuticsmd Inc | Composiciones farmacéuticas de estradiol insertadas por vía vaginal y métodos. |
| PL3525774T3 (pl) | 2016-10-11 | 2022-04-25 | Duke University | Leczenie lazofoksyfenem raka piersi er+ |
| WO2018071437A1 (fr) * | 2016-10-11 | 2018-04-19 | Sermonix Pharmaceuticals, Llc | Traitement au lasofoxifène de l'atrophie vulvovaginale (wa) et de l'ostéoporose chez des survivantes du cancer du sein ou d'autres malignités |
| RU2636619C1 (ru) * | 2017-02-20 | 2017-11-24 | Федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр акушерства, гинекологии и перинатологии имени академика В.И. Кулакова" Министерства здравоохранения Российской Федерации | Способ лечения вагинальной атрофии у женщин в постменопаузе с учетом состояния эпителия и микробиоценоза влагалища |
| CN112261937B (zh) | 2018-04-10 | 2023-11-14 | 杜克大学 | 乳腺癌的拉索昔芬治疗 |
| US11633405B2 (en) | 2020-02-07 | 2023-04-25 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical formulations |
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| CN117924262A (zh) * | 2022-10-14 | 2024-04-26 | 中国科学院上海药物研究所 | 二氢苯并噻喃类衍生物及其制备方法和用途 |
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| JPS63104924A (ja) * | 1986-10-20 | 1988-05-10 | Kanebo Ltd | 膣坐剤 |
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